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SecinH3 cytohesin inhibitor

Cat.No.S7685

SecinH3 is a selective cytohesin inhibitor with IC50 of 2.4 μM, 5.4 μM, 5.4 μM, 5.6 μM, 5.6 μM, and 65 μM for hCyh2, hCyh1, mCyh3, hCyh3, drosophila steppke, and yGea2-S7, respectively.
SecinH3 cytohesin inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 460.5

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Quality Control

Batch: S768501 DMSO]92 mg/mL]false]Ethanol]1 mg/mL]false]Water]Insoluble]false Purity: 99.62%
99.62

Cell Culture, Treatment & Working Concentration

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
LOX cells Antiinvasive assay 30 uM Antiinvasive activity against human LOX cells assessed as inhibition of 5% FBS-induced cell invasion at 30 uM by Matrigel based cell invasion assay ChEMBL
Click to View More Cell Line Experimental Data

Solubility

In vitro
Batch:

DMSO : 92 mg/mL (199.78 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 1 mg/mL

Water : Insoluble

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Mass Concentration Volume Molecular Weight
Dilution Calculator Molecular Weight Calculator

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
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Chemical Information, Storage & Stability

Molecular Weight 460.5 Formula

C24H20N4O4S

Storage (From the date of receipt)
CAS No. 853625-60-2 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles COC1=NN(C(=N1)C2=CC3=C(C=C2)OCO3)C4=CC=C(C=C4)NC(=O)CSC5=CC=CC=C5

Mechanism of Action

Targets/IC50/Ki
hCyh2
2.4 μM
hCyh1
5.4 μM
mCyh3
5.4 μM
hCyh3
5.6 μM
drosophila steppke
5.6 μM
yGea2-S7
65 μM
In vitro

In HepG2 cells, SecinH3 inhibits insulin signaling and associated gene expression. This compound also markedly inhibits migration of preadipocyte 3T3-L1 cells.

Kinase Assay
Aptamer displacement screen
A library of small molecules screened in duplicate from Comgenex (10000 molecules) in 386 well plates by fluorescence polarization at an excitation wavelength of 485 nm using read-out at 520 nm in a reaction volume of 50 μL at 37° C. The screening buffer is PBS, pH 7.5, 3 mM MgCl2, 100 nM fluorecein-labelled M69 aptamer, 1 μM cytohesin-1 Sec7 at 100 μM this compound concentrations.
In vivo

In mice, SecinH3 increases the expression of gluconeogenic genes, reduces the expression of glycolytic, fatty acid and ketone body metabolism genes in the liver, reduces liver glycogen stores, and increases plasma insulin. In mice bearing H460 xenografts, this compound significantly retards tumor growth through its antiproliferative and pro-apoptotic effect.

References

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